Synthesis and evaluation of novel biaryl oxazolidinones effective against gram-positive bacterial infections
摘要
Oxazolidinones are synthetic antibiotic class of compounds characterized by chemical structure, cyclic carbamate with ‘S’ configuration of substituent at C-5 position. The synthesis of oxazolidinones has gained increasing interest due to their unique mechanism of action that assures high antibiotic efficiency and low susceptibility to resistance mechanisms. Biaryl oxazolidinones are second-generation oxazolidinone (e.g. Tedizolid) having potency against multidrug-resistant (MDR) gram-positive pathogens including MRSA, VRE, penicillin-resistant S. pneumoniae and linezolid-resistant strains. The current manuscript covers structure activity based synthesis of 21 oxazolidinone analogs prepared through various chemical modifications. These novel biaryl oxazolidinones are prepared with the objective to increase spectrum of activity against multidrug-resistant Gram-positive bacteria.